Galectin-inhibitory thiodigalactoside ester derivatives have antimigratory effects in cultured lung and prostate cancer cells.

Tamara Delaine, Ian Cumpstey, Laurent Ingrassia, Marie Le Mercier, Paul Okechukwu, Hakon Leffler, Robert Kiss, Ulf Nilsson

Research output: Contribution to journalArticlepeer-review

Abstract

Aromatic 3,3'-diesters of thiodigalactoside were synthesized in a rapid three-step sequence from commercially available thiodigalactoside and evaluated as inhibitors of cancer- and immunity-related galectins. For each of galectins-1, -3, -7, and -9N-terminal domain, aromatic 3,3'-diesters of thiodigalactoside were found to have affinities in the low micromolar range, which represents a 7-70 fold enhancement over thiodigalactoside itself. No significant improvement was found for galectin-8 N-terminal domain. Two of the compounds were selected for testing in cell culture and were shown to have potent antimigratory effects on human PC-3 prostate and human A549 nonsmall-cell lung cancer cells.
Original languageEnglish
Pages (from-to)8109-8114
JournalJournal of Medicinal Chemistry
Volume51
Issue number24
DOIs
Publication statusPublished - 2008

Bibliographical note

The information about affiliations in this record was updated in December 2015.
The record was previously connected to the following departments: Division of Microbiology, Immunology and Glycobiology - MIG (013025200), Organic chemistry (S/LTH) (011001240)

Subject classification (UKÄ)

  • Medicinal Chemistry

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